• Develop a novel synthetic route of antimalarial drug piperaquine phosphate
• Prepare 500 gram of piperaquine phosphate
• Register a patent at National Office of Intellectual Property of Vietnam

Theoretical results:

A novel synthesis of piperaquine phosphate was developed using a cheaper reagent 1,3-propane diol ditosylate instead of toxic halogenated reagent 1,3-dibromopropane. Piperaquine phosphate was synthesized in 3 steps from 4,7-dichloroquinoline and piperazine in 50 gram scale with 54% overall yield.

505g of piperaquine phosphate was prepared using this method. The product of piperaquine phosphate was evaluated and passed the tests at National Drug Quality Control Institute. The synthetic route of piperaquin was submitted to National Office of Intellectual Property of Vietnam for a patent. We have received the acceptance letter number 71246/QĐ-SHTT on December, 13^th, 2012.

Applied results: The synthetic reagent 1,3-propane diol ditosylate was cheaper than the commercial, halogen reagent 1,3-dibromopropane the for production of piperaquine phosphate.

A novel synthesis of piperaquine phosphate was developed using a cheaper reagent 1,3-propane diol ditosylate instead of toxic halogenated reagent 1,3-dibromopropane. The synthetic steps was shortened and the overall yield is 54% from 4,7-dichloroquinoline and piperazine.

• Patents (list): “A synthetic route of Piperaquine”, submitted on September, 27^th, 2012. Acceptance letter from National Office of Intellectual Property of Vietnam number 71246/QĐ-SHTT on December, 13^th, 2012.
• Technological products (describe in details: technical characteristics, place): 505g of piperaquine phosphate, passed the tests at National Drug Quality Control Institute. Stored at Institute of Marine Biochemistry.